PDBsum entry 4brx

Transferase

PDB id: 4brx

Contents

Protein chain

260 a.a.

Ligands

KGW

SO4

Waters ×45

References listed in PDB file

Key reference

• Title: Synthesis of novel diarylamino-1,3,5-Triazine derivatives as fak inhibitors with anti-Angiogenic activity.
• Authors: P.Dao, R.Jarray, J.Le coq, D.Lietha, A.Loukaci, Y.Lepelletier, R.Hadj-Slimane, C.Garbay, F.Raynaud, H.Chen.
• Ref.: Bioorg Med Chem Lett, 2013, 23, 4552-4556. [DOI no: 10.1016/j.bmcl.2013.06.038]
• PubMed id: 23845217

Abstract

We report herein the synthesis of novel diarylamino-1,3,5-triazine derivatives as FAK (focal adhesion kinase) inhibitors and the evaluation of their anti-angiogenic activity on HUVEC cells. Generally, the effects of these compounds on endothelial cells could be correlated with their kinase inhibitory activity. The most efficient compounds displayed inhibition of viability against HUVEC cells in the micromolar range, as observed with TAE-226, which was designed by Novartis Pharma AG. X-ray crystallographic analysis of the co-crystal structure for compound 34 revealed that the mode of interaction with the FAK kinase domain is highly similar to that observed in the complex of TAE-226.